4-Anilinoquinoline triazines: A novel class of hybrid antimalarial agents

A novel class of hybrid 4-anilinoquinoline triazines have been synthesized and evaluated in vitro for their antimalarial activity against CQ-sensitive 3D7 strain of P. falciparum as well as for their cytotoxicity toward VERO cell line. Five compounds ( 19, 20, 23, 41 and 45) exhibited the antimalarial potency superior to CQ. Compounds 14 and 16 were found to be orally active at a dose of 100 mg/kg × 4 days against CQ-resistant strain of P. yoelii. Inhibition of β-hematin formation assay and molecular docking study has been conducted in order to gain insight into the mechanism of action of proposed targets for the 4-anilinoquinoline and triazine moiety of the hybrid compounds. A series of novel hybrid class 4-anilinoquinoline triazines have been synthesized and screened for their antimalarial activity in in vitro and in vivo assay. [Display omitted] ► A novel class of hybrid 4-anilinoquinoline triazines have been synthesized and evaluated in vitro for their antimalarial activity against CQ-sensitive 3D7 strain of P. falciparum. ► Five compounds ( 19, 20, 23, 41 and 45) exhibited the in vitro antimalarial potency superior to CQ. ► Compounds 14 and 16 were found to be orally active at a dose of 100 mg/kg × 4 days against CQ-resistant strain of P. yoelii.